RESUMO
CONTEXT: Polygonum hydropiper L. (Polygonaceae) (PH) is a traditional Chinese traditional medicine with a pungent flavor and mild drug properties. PH is mainly distributed in the channel tropism in the stomach and large intestine. PH has multiple uses and can be used to treat a variety of diseases for a long time. OBJECTIVE: This review summarizes the phytochemical and pharmacological activities, and applications of PH from 1980 to 2022. We also provide suggestions for promoting further research and developing additional applications of PH. METHODS: The data and information on PH from 1980 to 2022 reviewed in this article were obtained from scientific databases, including Science Direct, PubMed, Science Citation Index, SciFinder Scholar (SciFinder), Springer, American Chemical Society (ACS) Publications, and China National Knowledge Infrastructure (CNKI), etc. Some information was obtained from classic literature on traditional Chinese medicines. The search terms were Polygonum hydropiper, phytochemistry compositions of Polygonum hydropiper, pharmacological activities of Polygonum hydropiper, and applications of Polygonum hydropiper. RESULTS: The comprehensive analysis of the literature resulted in 324 compounds being isolated, identified, and reported from PH. Regarding traditional uses, the majority of phytochemical and pharmacological studies have indicated the diverse bioactivities of PH extracts, flavonoids, and volatile oil elements, including antibacterial, antifungal, insecticidal, antioxidant, and anti-inflammatory. CONCLUSIONS: PH has a long history of diversified medicinal uses, some of which have been verified in modern pharmacological studies. Further detailed studies are required to establish scientific and reasonable quality evaluation standards and action mechanisms of active constituents from PH.
Assuntos
Óleos Voláteis , Polygonum , Polygonum/química , Medicina Tradicional Chinesa , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , EtnofarmacologiaRESUMO
OBJECTIVE: Vigabatrin (VGB) is the first-line treatment for infantile spasms (IS). Previous studies have shown that VGB exposure may cause vigabatrin-associated brain abnormalities on magnetic resonance imaging (MRI) (VABAM). Based on previous studies, this study aimed to go further to explore the possible risk factors and the incidence of VABAM. In addition, diffusion-weighted imaging (DWI) and T2-weighted imaging (T2WI) were compared to explore whether DWI should be used as a routine examination sequence when MRI is performed in children receiving VGB. METHODS: Children with IS receiving VGB were selected as the study subjects. Whether VABAM occurred or not was categorized as the VABAM group and the non-VABAM group, respectively. Their general clinical data and medication exposure were collected. The possible risk factors of VABAM and different MRI sequences were compared and statistically analyzed. RESULTS: A total of 77 children with IS were enrolled in the study, of which 25 (32.5%) developed VABAM. Twenty-three of the 25 VABAM cases have a peak dosage of VGB between 50 and 150 mg/kg/day. The earliest observation time of VABAM was 30 days. Regression analysis of relevant risk factors showed that the peak dosage of VGB was the risk factor for VABAM. Comparison between different MRI sequences showed that DWI is more sensitive than T2WI to the evaluation of VABAM. SIGNIFICANCE: In our study, the occurrence of VABAM was 32.5%, indicating a higher incidence than in most previous reports. In addition, we once again verified that the peak dosage of VGB was the risk factor of VABAM. Caution should be exercised that our data also suggest that VABAM may occur even using the conventional dosage of VGB (ie, 50-150 mg/kg/day). Therefore, even when using the conventional dosage of VGB, regular MRI examination should be required. Furthermore, DWI sequence should be used as a routine examination sequence when MRI is performed in children with IS who are receiving VGB.
Assuntos
Espasmos Infantis , Vigabatrina , Anticonvulsivantes/efeitos adversos , Encéfalo/diagnóstico por imagem , Criança , Humanos , Imageamento por Ressonância Magnética , Estudos Retrospectivos , Espasmos Infantis/induzido quimicamente , Espasmos Infantis/diagnóstico por imagem , Espasmos Infantis/tratamento farmacológico , Vigabatrina/efeitos adversosRESUMO
PURPOSE: There was no evidence whether the mammalian/mechanistic target of rapamycin pathway hyperactivation and long-term use of mTOR inhibitors have any effects on the physical development of children. The aim was to evaluate these effects by comparing the physical development of children with TSC and normal children. METHODS: A total of 120 eligible children were enrolled. They were administered sirolimus and followed for at least 12 months. Height, weight, BMI and lipid metabolism index were collected during treatment. Pearson's chi-square and Fisher's exact test were used for comparison of proportions of patients exhibiting normal and abnormal physical growth before and after 1 year of treatment. Logistic regression was used to evaluate the influence of age, sex and abnormal lipid metabolism on the increased BMIs of TSC patients after treatment. RESULTS: Most of the enrolled TSC children were in the normal height, weight and BMI ranges at baseline (91.7%, 95.8% and 78.3%, respectively). Most remained in the normal height, weight and BMI ranges after 1 year of sirolimus treatment (94.2%, 95% and 76.7%, respectively). There was no significant difference in the proportion of physical development before and after treatment (p > 0.05). Thirty-eight (38/106, 35.8%) patients had increased BMIs after 1 year of treatment, but there was no significant correlation between age, sex and lipid metabolism and increased BMI. CONCLUSIONS: Overactivation of the mTOR pathway and long-term administration of sirolimus does not affect the physical development of children with TSC.
Assuntos
Esclerose Tuberosa , Animais , Criança , Humanos , Mamíferos , Sirolimo/efeitos adversos , Esclerose Tuberosa/tratamento farmacológicoRESUMO
Based on the theory of activating spleen and generating blood, this study explored the effect of Rehmanniae Radix Prae-parata on the spleen metabolome of the rat model with blood deficiency syndrome.The rat model of blood deficiency syndrome was established by combining with cyclophosphamide(CTX) and N-acetyl-phenylhydrazine(APH), and the metabolomes of the spleen samples were analyzed with ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS).Principal component analysis(PCA) and orthogonal partial least squares-discriminant analysis(OPLS-DA) were carried out for the metabolite profiles of spleen samples.The MEV heatmap and metabolic network were established based on the potential biomarkers.Finally, the blood routine indexes were combined with the metabolomic profile to reveal the mechanism of Rehmanniae Radix Praeparata in activating spleen and generating blood.The treatment with CTX and APH decreased the blood routine indexes such as white blood cell count(WBC), red blood cell count(RBC), platelet(PLT), and hematocrit(HCT), indicating that the rat model of blood deficiency syndrome was successfully established.The administration of Rehmanniae Radix Praeparata significantly improved the blood routine indexes, which suggested that Rehmanniae Radix Praeparata played a role in replenishing blood.In addition, the metabolomics analysis identified 41 potential biomarkers.The PCA and MEV heatmap also showed significant improvement effect of Rehmanniae Radix Praeparata on the spleen metabolic profile.These potential biomarkers were mainly involved in tricarboxylic acid cycle, niacin and nicotinamide metabolism, phenylalanine metabolism, tyrosine metabolism, taurine and hypotaurine metabolism, and sphingolipid metabolism.Therefore, we hypothesize that Rehmanniae Radix Praeparata may regulate energy metabolism, peripheral blood production, and oxidative injury of hemocytes to tonify blood.
Assuntos
Medicamentos de Ervas Chinesas , Animais , Biomarcadores , Medicamentos de Ervas Chinesas/farmacologia , Metabolômica , Extratos Vegetais , Ratos , Rehmannia , BaçoRESUMO
This paper clarified the scientific connotation of the changes in cold and heat properties of Arisaematis Rhizoma and Arisaema Cum Bile through investigating the changes of substance and energy metabolism after drug intervention in the rats with normal and cold/heat syndrome, so as to improve the method of evaluating the drug properties of Chinese medicine. After one week of adaptive feeding, healthy male SD rats were randomly divided into three parts: normal rats, heat syndrome rat models, and cold syndrome rat models. Through ice water bath and oral euthyrox(120 µg·kg~(-1)), the models of cold syndrome and heat syndrome were induced, respectively. The models were made at 9:00 am. and administrated by gavage at 3:00 pm. every day. All administration groups were administrated with Arisaematis Rhizoma and Arisaema Cum Bile decoction, respectively, and the blank group was given the same dose of normal saline. After continuous administration for 15 d, the rats were anesthetized by chloral hydrate, blood was taken from abdominal aorta, and the hearts and livers were removed and stored at-80 â. The changes in the body weight and anal temperature of rats during administration were detected, and the liver coefficient of rats was detected after removing the liver. Enzyme-linked immunosorbent assay(ELISA) was adopted to detect the expression level of the indexes related to substance and energy metabolism in liver and heart of rat, and Western blot was used to detect the expression of key proteins in AMPK/mTOR signaling pathway for further verification. The results showed that Arisaematis Rhizoma enhanced the expression level of enzymes related to substance and energy metabolism in the normal and cold and heat syndrome rat models, and increased anal temperature, which exhibited warm(hot) drug property. Arisaema Cum Bile inhibited the level of substance and energy metabolism in rats, and reduced anal temperature, which showed cold(cool) drug property. Chinese Pharmacopoeia has recorded "Arisaematis Rhizoma has warm property and Arisaema Cum Bile has cool property", which is consistent with the phenomenon in this study. Therefore, it is feasible to evaluate the drug properties of Chinese medicine based on the substance and energy metabolism of normal and cold/heat syndrome model rats, which completes the method of evaluating drug properties of Chinese medicine.
Assuntos
Arisaema , Resposta ao Choque Frio , Medicamentos de Ervas Chinesas , Golpe de Calor , Proteínas Quinases Ativadas por AMP , Animais , Arisaema/química , Bile , Hidrato de Cloral , Resposta ao Choque Frio/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Metabolismo Energético , Golpe de Calor/terapia , Temperatura Alta , Masculino , Ratos , Ratos Sprague-Dawley , Solução Salina , Síndrome , Serina-Treonina Quinases TOR , Tiroxina , ÁguaRESUMO
A UPLC-MS/MS method was developed and validated the determination and pharmacokinetic study of magnoflorine, cauloside C, hederagenin, and oleanolic acid from Caulophyllum robustum. Digoxin was used as the internal standard. The pretreated plasma samples were carried out on a Waters ACQUITYUPLC HSS T3 column at 35 °C with a mobile phase of acetonitrile-water (90:10, v/v) at a flow rate of 0.2 mL/min. This article describes the most simple, sensitive, and validated UPLC-MS/MS method to date for the simultaneous successful determination of four compounds in rat plasma after oral administration of the extract of C. robustum and their pharmacokinetic studies.
Assuntos
Caulophyllum , Administração Oral , Animais , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Estrutura Molecular , Plasma , Ratos , Espectrometria de Massas em TandemRESUMO
This paper aimed to explore the mechanism of the split components of Phytolaccae Radix by means of network pharmaco-logy. Based on the theoretical hypothesis of the nature and taste of traditional Chinese medicine, the chemical components of the separated components of Phytolaccae Radix were selected by using Traditional Chinese Medicine Systems Pharmacology Database(TCMSP) and Traditional Chinese Medicines IntegratedDatabase(TCMID) databases in combination with related literatures. Relevant target analysis was carried out based on PubChem and SwissTargetPrediction databases. Targets corresponding to disease were excavated based on GeneCards for each split component, corresponding potential targets were obtained through mapping the target set of target compounds to disease targets. GO biological process analysis and KEGG pathway enrichment analysis were performed on the mapped targets with the help of DAVID database. Based on Cytoscape software and the corresponding efficacy, the network diagram of "medicinal material-split components-compound-target-pathway" was constructed to explore the mechanism of different efficacy of the separated components of Cytoscape. And the target purgation and diuretic mapping was used as the target of the traditional efficacy of smoothening secretion for the first time. The study explored esculentoside component, fatty oil component and phenolic acid component, a total of 30 target compounds and 301 corresponding targets, involving 44 potential targets for "anti-inflammatory", 50 potential targets for "immunoregulation", 52 potential targets for "smoothening secretion", 28 potential targets for "antibacterial activity", 28 potential targets for "antiviral effect", and 29 potential targets for "antitumor effect". Topological analysis revealed 14 key gene targets such as MAPK8, MAPK14, EGFR and PTGS2. A total of 684 GO entries and 235 KEGG pathways were obtained through bioinformatics enrichment analysis, mainly involving TNF signaling pathway, NF-kappaB signaling pathway and MAPK signaling pathway. This study revealed the multi-component, multi-target, and multi-channel action mechanism of the split components of Phytolaccae Radix, which provided certain basis for the next step to clarify the split components of Phytolaccae Radix through the method of system biology, and injected new content and significance into the study of properties and flavors theory.
Assuntos
Medicamentos de Ervas Chinesas , Medicamentos de Ervas Chinesas/farmacologia , Medicina Tradicional Chinesa , Transdução de Sinais , SoftwareRESUMO
In this paper, the extraction rate of crude polysaccharides and the yield of polysaccharides from Hippocampus served as test indicators. The comprehensive evaluation indicators were assigned by the R language combined with the entropy weight method. The Box-Behnken design-response surface methodology(BBD-RSM) and the deep neural network(DNN) were employed to screen the optimal parameters for the polysaccharide extraction from Hippocampus. These two modeling methods were compared and verified experimentally for the process optimization. This study provides a reference for the industrialization of effective component extraction from Chinese medicinals and achieves the effective combination of modern technology and traditional Chinese medicine.
Assuntos
Carboidratos da Dieta , Polissacarídeos , Hipocampo , Redes Neurais de Computação , TemperaturaRESUMO
How to accelerate tendon healing remains a clinical challenge. In this study, a suture carrying nanoparticle/pEGFP-basic fibroblast growth factor (bFGF) and pEGFP-vascular endothelial growth factor A (VEGFA) complexes was developed to transfer the growth factor genes into injured tendon tissues to promote healing. Polydopamine-modified sutures can uniformly and tightly absorb nanoparticle/plasmid complexes. After tendon tissues were sutured, the nanoparticle/plasmid complexes still existed on the suture surface. Further, we found that the nanoparticle/plasmid complexes delivered into tendon tissues could diffuse from sutures to tendon tissues and effectively transfect genes into tendon cells, significantly increasing the expression of growth factors in tendon tissues. Finally, biomechanical tests showed that nanoparticle/pEGFP-bFGF and pEGFP-VEGFA complex-coated sutures could significantly increase the ultimate strengths of repaired tendons, especially at 4 weeks after operation. Two kinds of nanoparticle/plasmid complex-coated sutures significantly increased flexor tendon healing strength by 3.7 times for Ethilon and 5.8 times for PDS II, respectively, compared with the corresponding unmodified sutures. In the flexor tendon injury model, at 6 weeks after surgery, compared with the control suture, the nanoparticle/plasmid complex-coated sutures can significantly increase the gliding excursions of the tendon and inhibit the formation of adhesion. These results indicate that this nanoparticle/plasmid complex-coated suture is a promising tool for the treatment of injured tendons.
Assuntos
Materiais Revestidos Biocompatíveis , Técnicas de Transferência de Genes , Nanopartículas , Suturas , Traumatismos dos Tendões/genética , Traumatismos dos Tendões/terapia , Transgenes , Cicatrização , Animais , Sobrevivência Celular , Materiais Revestidos Biocompatíveis/química , Modelos Animais de Doenças , Liberação Controlada de Fármacos , Expressão Gênica , Terapia Genética , Cinética , Nanopartículas/química , Nanopartículas/ultraestrutura , Plasmídeos/genética , Transgenes/genética , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo , Cicatrização/genéticaRESUMO
A simple and sensitive analysis using ultra high performance liquid chromatography with a tandem mass spectrometric system operated in selected reaction monitoring mode was developed for the determination of 11 phenolic acids, atractyloside, and carboxyatractyloside in rat plasma. The two classes of analytes were then separated on a Waters ACQUITY™ UPLC HSS T3 column (50 mm × 2.1 mm, 1.8 µm) using gradient elution with a mobile phase of 0.2% formic acid in water containing 10 mM ammonium acetate and methanol. Detection was accomplished by selected reaction monitoring scanning via an electrospray source operating in negative ionization mode. The calibration curve was linear (R2 = 0.990) over a concentration range of 1.20-3500 ng/mL, while the validated lower limit of quantification was 1.20 ng/mL. The precision varied from 0.84 to 4.62%, and the accuracy varied within ±5%. The method proved robust with sample freezing and thawing and with short- and long-term sample storage. The established method was used for simultaneous quantification and was successfully used for the first time for the pharmacokinetic evaluation of 13 compounds after the intragastric administration of raw and processed Fructus Xanthii in rats. The results indicated that processing affects the absorption and metabolism of Fructus Xanthii extract. Importantly, the results also indicated the importance of processing for the clinical application of traditional Chinese medicine.
Assuntos
Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/farmacocinética , Administração Oral , Animais , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Masculino , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em TandemRESUMO
This project is to investigate lignans from the dried fruits of Xanthium sibiricum (Xanthii Fructus). The chemical constituents were extract by 70% ethanol and isolated by silica gel, ODS, Sephadex LH-20, MCI column chromatography. Based on comparison of their spectral data with those reported in literature, they were elucidated as (-)-pinoresinol (1), balanophonin A (2), diospyrosin (3), dehydrodiconiferyl alcohol (4), 2-(4-hydroxy-3-methoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol (5), (-)-simulanol (6), (-)-7R,8S-dehydrodiconiferyl alcohol (7), chushizisin E (8), dihydrodehydrodiconiferyl alcohol (9), 7R,8S-dihydrodehydrodiconiferyl alcohol 4-O-ß-D-glucopyranoside (10), erythro-1,2-bis(4-hydroxy-3-methoxyphenyl)-1,3-propanediol (11), leptolepisol D (12), 8-O-4' neolignan 4-O-ß-glucopyranoside (13), (-)-1-O-ß-D-glucopyranosyl-2-{2-methoxy-4-[1-(E)-propen-3-ol]phenoxyl}-propane-3-ol(14), 1-(4-hydroxy-3-methoxy)-phenyl-2-[4-(1,2,3-trihydroxypropyl)-2-methoxy]-phenoxy-1,3-propandiol (15), threo-dihydroxy dehydrodiconiferyl alcohol (16), (-)-(2R)-1-O-ß-D-glucopyranosyl-2-{2-methoxy-4-[(E)-formylviny1]phenoxyl} propane-3-ol (17). Compound 2-17 were isolated from the genus Xanthium for the first time. Compound 1 were isolated form Xanthii Fructus for the first time.
Assuntos
Frutas/química , Lignanas/análise , Xanthium/química , Compostos Fitoquímicos/análiseRESUMO
There is no doubt that the traditional Chinese medicine(TCM) is effective, practical and scientific after it was used for thousands of years. However, the mechanisms of action of many TCM are still unclear because of their multi-component, multi-target and multi-level features, which hinder the modernization and internationalization of the TCM. Proteomics is to analyze the composition and activity of intracellular proteins which are changing dynamically from a holistic perspective. It is consistent with the holistic and dynamic views of the TCM and brings about the hope of clarifying the mechanism of action of the TCM. In recent years, great progress has been made in the application of proteomics to determine the mechanism of the TCM. This article introduced the core technologies of proteomics and systematically summarized the applications of proteomics in the study of the mechanism of the Chinese medicinal formulae, single Chinese medicine and monomeric compounds from the TCM to provide innovative ideas and methods for reference.
Assuntos
Medicina Tradicional Chinesa , Proteômica , Medicamentos de Ervas ChinesasRESUMO
Graphitic carbon nitride (g-C3N4) has been widely studied as a metal-free photocatalyst, leading to some excellent results; however, the rapid recombination of photogenerated charge carriers substantially limits its performance. Here, we establish two types of g-C3N4-based heterojunction (type II and nonmediator assisted Z-scheme) photoanodes on a transparent conducting substrate via coupling with rod-like and nanoparticulate WO3, respectively. In these composites, g-C3N4 film grown by electrophoretic deposition of exfoliated g-C3N4 serves as the host or guest material. The optimized type II WO3/g-C3N4 composite exhibits an enhanced photocurrent of 0.82 mA cm-2 at 1.23 V vs. RHE and an incident photo-to-current conversion efficiency (IPCE) of 33% as compared with pure WO3 nanorods (0.22 mA cm-2 for photocurrent and 15% for IPCE). Relative to pure g-C3N4 film (with a photocurrent of several microampere and an IPCE of 2%), a largely improved photocurrent of 0.22 mA cm-2 and an IPCE of 20% were acquired for the Z-scheme g-C3N4/WO3 composite. The enhancement can be attributed to accelerated charge separation in the heterointerface because of the suitably aligned band gap between WO3 and g-C3N4, as confirmed by optical spectroscopy and ultraviolet photoelectron spectroscopy (UPS) analysis. The photocatalytic process and mechanism of the g-C3N4-based heterojunctions are proposed herein, which potentially explain the origin of the enhanced photoelectrochemical performance. This achievement and the fundamental information supplied here indicate the importance of rationally designing heterojunction photoelectrodes to improve the performance of semiconductors. This is particularly important for materials such as pure g-C3N4 and WO3, as their photoactivities are strongly restricted by high recombination rates.
RESUMO
Bradysia odoriphaga Yang and Zhang is the primary insect pest that affects Chinese chive in northern China. Nevertheless, very few studies have been conducted on the use of chitin synthesis inhibitors (CSIs) for the control of B. odoriphaga. Here, lethal and sublethal effects of the CSI chlorfluazuron on B. odoriphaga were studied to explore the use for integrated pest management (IPM) of B. odoriphaga. A contact and ingestion toxicity bioassay showed that chlorfluazuron was more active against B. odoriphaga than three other CSIs, with a 72h LC50 of 0.1593mg/L. Treatment with the LC50 dose of chlorfluazuron decreased both the intrinsic and finite rates of increase of B. odoriphaga, in addition to reproduction rate, survival rate, and fecundity, and the mean generation time, total preovipositional period and larval development duration were shortened, compared with those of the control and LC10 groups. The mean generation time, total preovipositional period and larval development duration were all also markedly decreased by treatment with chlorfluazuron at the LC10. Furthermore, chlorfluazuron inhibited the feeding of the final instar larvae for a short period. Glutathione S-transferase and microsomal mixed function oxidase activities increased after exposure to the chemical. These results showed that chlorfluazuron at the sublethal LC50 treatment inhibited B. odoriphaga population growth, whereas the danger of causing rapid population growth by using a lower sublethal concentration was demonstrated with the sublethal LC10 treatment. Therefore, chlorfluazuron should be used with caution in an IPM program for B. odoriphaga.
Assuntos
Quitina/antagonistas & inibidores , Dípteros/efeitos dos fármacos , Inseticidas/toxicidade , Compostos de Fenilureia/toxicidade , Piridinas/toxicidade , Animais , Quitina/biossíntese , Dípteros/metabolismo , Dípteros/fisiologia , Feminino , Glutationa Transferase/metabolismo , Proteínas de Insetos/metabolismo , Larva/efeitos dos fármacos , Larva/metabolismo , Larva/fisiologia , Masculino , Oxigenases de Função Mista/metabolismo , Reprodução/efeitos dos fármacosRESUMO
Three new lignans (1 - 3), together with four new thymoquinol glycosides (4 - 7), were isolated from 70%-EtOH extract of the rattan stems of Schisandra chinensis. The structures of 1 - 7 were elucidated by detailed spectroscopic analyses, and these new compounds were identified as pinobatol-9-O-ß-d-glucopyranoside (1), 1,2,13,14-tetramethoxydibenzocyclooctadiene 3,12-O-ß-d-diglucopyranoside (2), 3,7-dihydroxy-1,2,13,14-tetramethoxydibenzocyclooctadiene 12-O-ß-d-glucopyranoside (3), thymoquinol 2-O-ß-d-apiofuranosyl-(1â6)-ß-d-glucopyranoside (4), thymoquinol 2-O-α-d-arabinofuranosyl-(1â6)-ß-d-glucopyranoside (5), thymoquinol 5-O-ß-d-apiofuranosyl-(1â6)-ß-d-glucopyranoside (6), and thymoquinol 5-O-α-d-arabinofuranosyl-(1â6)-ß-d-glucopyranoside (7). The neuroprotective activity of 1 - 7 was evaluated on PC12 cells with neurotoxicity induced by amyloid-beta 1 - 42 (Aß1 - 42 ). Compounds 2 and 3 showed protecting activity against Aß-induced toxicity in PC12 cells.
Assuntos
Benzoquinonas/farmacologia , Ciclo-Octanos/farmacologia , Glicosídeos/farmacologia , Lignanas/farmacologia , Fármacos Neuroprotetores/farmacologia , Caules de Planta/química , Schisandra/química , Peptídeos beta-Amiloides/antagonistas & inibidores , Peptídeos beta-Amiloides/toxicidade , Animais , Benzoquinonas/química , Benzoquinonas/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Octanos/química , Ciclo-Octanos/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Lignanas/química , Lignanas/isolamento & purificação , Estrutura Molecular , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/isolamento & purificação , Células PC12 , Fragmentos de Peptídeos/antagonistas & inibidores , Fragmentos de Peptídeos/toxicidade , RatosRESUMO
A ultra-high performance liquid chromatography-electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) method was successfully developed and validated for the identification and determination of eight alkaloids: tetrahydropalmatine (A); palmatine (B); magnoflorine (C); columbamine (D); berberine (E); worenine (F); berberrubine (G) and coptisine (H) in rat plasma, which are the active components in Coptis deltoidea C. Y. cheng et Hsiao (CCY) and Coptis chinensis Franch (CF). The chromatographic separation of analytes was successfully achieved on an Agilent SB-C18 column (1.8 µm, 150 mm × 2.1 mm) using a programme with a mobile phase consisting of acetonitrile and water containing 0.3% acetic acid at a flow rate of 0.25 mL/min. The analytes were detected with a triple quadrupole tandem MS in multiple reaction monitoring (MRM) mode and an electrospray ionization (ESI) source in positive mode. The validated method showed good linearity over a wide concentration range (r² > 0.991), and lower limits of quantification (LLOQ) less than 1.1 ng/mL for all analytes, and matrix effects ranged from 85.2% to 106.8%. The mean extraction recoveries were no less than 86.4%, and the precision and accuracy were within the acceptable limits. All analytes were proven to be stable during sample storage and analysis procedures. The method validation results demonstrated that the proposed method was sensitive, specific, and reliable, which could lay a foundation for the pharmacokinetic study of eight analytes after oral administration of CCY and CF in subsequent studies.
Assuntos
Alcaloides/química , Alcaloides/farmacocinética , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacocinética , Espectrometria de Massas em Tandem , Administração Oral , Alcaloides/administração & dosagem , Animais , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Masculino , Ratos , Reprodutibilidade dos Testes , Sensibilidade e EspecificidadeRESUMO
Dioscoreae Bulibferae Rhizoma (RDB) is commonly used in clinical Chinese medicine. It has been used in many kinds of traditional Chinese medicine (TCM), but the toxicity of RDB, easily leads to hepatotoxicity. The objective of the present study is to investigate the synergistic protective effect of Scutellariae Radix (SR) with Phellodendri Chinensis Cortex (PCC) on RDB caused liver toxicity in rats. SD female rats were adopted to establish the hepatotoxicity models by RDB (9 gâ¢kg⻹, ig) once daily for 28 consecutive days. After 28 days, liver histological changes were observed, and the activity of transaminase and antioxidant enzymes was evaluated. Morphological and biochemical indicators evaluation showed that, Dioscoreae Bulibferae Rhizoma-induced hepatotoxicity models were successful, and the liver cells were dissolved and swelling with fatty degenerationï¼ inflammatory cells were present in gaps; local punctiformed or lamellar hydropic degeneration was found in liver tissues, with partial necrosis. Indexes of liver function (ALT, AST and ALP) were significantly increased (P<0.05 or P<0.01). The combination of SR and PCC has protective effect on RDB-induced hepatotoxicity in rats. SR+PCC exerted the strongest protective effects against RDB-induced hepatotoxicity. SR, PCC, and SB+CP were observed to exhibit hepatoprotective effect as demonstrated by significant decrease in serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) (P<0.05 or P<0.01), and MAD level in liver tissue (P<0.001), significant increase in GSH content in liver tissue (P<0.001), and significant improvement in his to pathologic changes of liver tissues in rats. SR, PCC and their combinations could achieve liver protection effect by reducing ALT, ALP and AST level in serum, increasing GSH level and anti-oxidantability of liver tissues, and reducing hepatic tissue cells injury.
Assuntos
Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Dioscorea/toxicidade , Medicamentos de Ervas Chinesas/administração & dosagem , Phellodendron/química , Scutellaria baicalensis/química , Alanina Transaminase/metabolismo , Animais , Aspartato Aminotransferases/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/enzimologia , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Dioscorea/química , Sinergismo Farmacológico , Medicamentos de Ervas Chinesas/toxicidade , Humanos , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Ratos , Ratos Sprague-Dawley , Rizoma/química , Rizoma/toxicidadeRESUMO
Coptidis Rhizoma is commonly used in clinical medicine. It has been widely used in traditional Chinese medicine (TCM), with the functions of clearing heat, drying dampness, purging intense heat relieve toxins. However, the herb contains complex ingredients, and CYP450 isoenzyme is the main metabolic enzyme of the drug, so it is of important clinical significance to study the effect of Coptidis Rhizoma on cytochrome P450 enzymes. In the experiment, liver tissues of rats were selected and liver microsomes were separated by differential centrifugation. Bicinchoninic acid (BCA) Protein quantitation was done by enzyme linked immunosorbent assay, and iTRAQ (isobaric tags for relative and absolute quantification) was combined with the 2D-LC-MS/MS analysis method for identification of CYP450 proteins. With Coptidis Rhizoma, 30 CYP450 isoenzymes were identified, with 7 proteins significantly increased and 8 decreased in response to Coptidis Rhizoma, while the rest 15 had no change. iTRAQ technology combined with 2D-LC-MS/MS method could be used to comprehensively study CYP450 enzyme, but it is necessary to further evaluate in vitro levels of Coptidis Rhizoma and avoid any potential clinical drug-drug interaction.
Assuntos
Cromatografia Líquida/métodos , Coptis/química , Sistema Enzimático do Citocromo P-450/genética , Medicamentos de Ervas Chinesas/administração & dosagem , Proteômica/métodos , Espectrometria de Massas em Tandem/métodos , Animais , Sistema Enzimático do Citocromo P-450/metabolismo , Feminino , Isoenzimas/genética , Isoenzimas/metabolismo , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/enzimologia , Ratos , Rizoma/químicaRESUMO
In this study, the chemical constituentsfrom Valeriana amurensis AD-effective fraction were investigated based on the effect of Valeriana amurensis on Alzheimer's disease (AD) in previous study. Valeriana amurensis was extracted with 75% ethanol and the obtained extract were extracted and subjected to AB-8 macroporous resin column to obtain the AD-effective fraction of Valeriana amurensis. 9 compounds (1-9) were isolated with silica gel, ODS column chromatography and preparative HPLC. The structures of these compounds were determined as 6-hydroxy-7-(hydroxymethyl)-4-methylenehexahydrocyclopenta[c]-pyran-1(3H)-one (1), suspensolide F (2), loganin(3), α-morroniside(4), ß-morronisid (5), partinovalerosidate (6), zansiumloside A (7), (-)-angelicoidenol-2-O-ß-D-glucopyranoside (8), citroside A (9). Compounds 6-9 were isolated from the valerian genus for the first time and further investigated the anti-AD effect of compounds 1-9 in vitro found that compound 2 and 6 protected the PC12 cells from injury significantly.
Assuntos
Doença de Alzheimer/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Valeriana/química , Animais , Cromatografia Líquida de Alta Pressão , Células PC12 , RatosRESUMO
Twelve xanthones compounds were isolated from the ethanol extract of Gentianella acuta by means of reversed-phase preparative HPLC and various kinds of column chromatography including silica gel and ODS . Their structures were fully elucidated on the basis of MS, 1D and 2D-NMR data. The structures of xanthones were identified as 1, 7-dihydroxy-3-methoxyxanthone-7-O-ß-D-glucopyranoside (1), swertiapuniside (2), 1, 3, 8- trihydroxy -4, 5-dimethoxyxanthone-1-O-ß-D-glucopyranosyl(6â1)-O-ß-D-glucopyranoside (3), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone-2-O-ß-D-glucopyranoside (4), 1, 3, 7, 8-tetrahydroxyxanthone-1-O-ß-D-glucopyranoside (5), 1, 3, 5, 8-tetrahydroxy-5, 6, 7, 8-tetrahydroxanthone (6), 1, 3, 5-thihydroxyxanthone (7),1, 3, 5, 8-tetrahydroxyxanthone (8), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone (9), bellidifolin (10), mangiferin (11), swertianolin (12). Compounds 1-9 were isolated from Gentianella genus for the first time.